Publication

Polycyclic Peptide Therapeutics

Related publications (34)

Generation of photoswitchable peptide ligands by phage display

Photoswitchable ligands are used to control and study complex biological systems such as folding of proteins and peptides, enzymatic reactions or neuronal signaling. They are typically developed by conjugating photochromic compounds to known ligands so tha ...

EPFL2015

Phage Selection of Bicyclic Peptides and High-Throughput Screening of Chemical Compounds for the Identification of Novel Inhibitors of the Notch Pathway

Notch signaling is a highly conserved developmental pathway that plays important roles in the regulation of cellular processes including cell fate decisions and stem cell maintenance. A tight regulation of the Notch cascade ensures proper tissue homeostasi ...

EPFL2015

Exploring Ligand Affinities for Proteins by NMR of Long-Lived States

Roberto Buratto

The detection of molecules that can bind to active sites of protein targets and the measurement of their affinities is a promising application of NMR. Nowadays, the screening of drug candidates is routinely done by NMR in pharmaceutical industry. We have p ...

EPFL2015

Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles

Sara Vigne

Polymer-block-peptide conjugates are tailored to render hydrophobic small molecule drugs water soluble. The combinatorial strategy selects for bioconjugates that exhibit sequence-specific solubilization and switchable release profiles of the cargo through ...

Wiley-V C H Verlag Gmbh2015

Improving Bicyclic Peptide Phage Display and Development of Sortase A Inhibitors

Inmaculada Rentero Rebollo

Bicyclic peptide ligands are promising molecules for the development of new therapeutics. They combine advantages from large protein therapeutics and small molecule drugs. Large combinatorial libraries of bicyclic peptides can be generated and screened by ...

EPFL2014

Phage Selection of Photoswitchable Peptide Ligands

Christian Heinis, Inmaculada Rentero Rebollo, Shiyu Chen, Silvia Bellotto, Hermann A. Wegner

Photoswitchable ligands are powerful tools to control biological processes at high spatial and temporal resolution. Unfortunately, such ligands exist only for a limited number of proteins and their development by rational design is not trivial. We have dev ...

American Chemical Society2014

Development of bicyclic peptide Her2 binders and phage selection of alpha-helical peptide ligands

Philippe Diderich

Conformationally constrained peptide ligands offer an attractive format for the development of therapeutics. They can bind with high affinity and selectivity to protein targets, they are small enough to diffuse into tissues, they can be synthesized chemica ...

EPFL2014

Directed Evolution of Bicyclic Peptides for Therapeutic Application

Christian Heinis, Philippe Diderich

Many naturally occurring cyclic peptides or derivatives thereof are used as therapeutics such as the human hormones vasopressin and oxytocin or the antibiotics vancomycin and daptomycin. The success of cyclic peptide therapeutics is based on their ability ...

Schweizerische Chemische Gesellschaft2013

Detection of Drug-Protein Interactions with an Improved Yeast Three-Hybrid System

Cindy Fellay

The identification of the targets of therapeutic drugs is one of the major challenges for pharmaceutical companies. The main target responsible for drug action is often known, but most drugs also bind other targets, either causing deleterious side effects ...

EPFL2013

Phage selection of bicyclic peptides

Christian Heinis, Inmaculada Rentero Rebollo

Bicyclic peptides are small, constrained peptides that can bind with high affinity and selectivity to protein targets. Their small size provides a number of advantages over larger protein-based ligands, including access to chemical synthesis, better tissue ...

Academic Press Inc Elsevier Science2013

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